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Synthesis, Antibacterial Activity, and Docking Studies of 1,2,3‐triazole‐tagged Thieno[2,3‐ d ]pyrimidinone Derivatives
Author(s) -
Aruna Kumari M.,
Triloknadh S.,
Harikrish.,
Vijjulatha M.,
Venkata Rao C.
Publication year - 2017
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2995
Subject(s) - chemistry , bacillus subtilis , antibacterial activity , bacillus cereus , klebsiella pneumonia , escherichia coli , stereochemistry , enterobacter aerogenes , docking (animal) , bacteria , biochemistry , medicine , genetics , nursing , biology , gene
Novel (1‐(substituted phenyl)‐1 H ‐1,2,3‐triazol‐4‐yl)methyl‐2‐(4‐oxo‐5,6,7,8‐tetrahydrobenzo[1,2]thieno[2,3‐ d ]pyrimidin‐3(4 H )‐yl)acetate derivatives were synthesized. All the compounds showed significant antibacterial activity against Gram‐negative ( Escherichia coli and Klebsiella pneumonia ) and Gram‐positive ( Bacillus subtilis and Bacillus cereus ) bacteria. Particularly, (1‐(3‐nitrophenyl)‐1 H ‐1,2,3‐triazol‐4‐yl)methyl‐2‐(4‐oxo‐5,6,7,8‐tetrahydrobenzo[1, 2]thieno[2,3‐ d ]pyrimidin‐3(4 H )‐yl)acetate was found to be most potent against E. coli , K. pneumonia , and B. subtilis with MIC 25 μg/ml . Molecular docking was also performed on purine riboswitch of B. subtilis and thiamine pyrophosphate riboswitch of E. coli .